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Document Page 117 53. Carteau S, Mouscadet JF, Goulaouic H, Subra F, Auclair C. Inhibitory effect of the polyanionic drug suramin on the in vitro HIV DNA integration reaction. Arch Biochem Biophys 1993; 305:606–610. 54. Li CJ, Zhang LJ, Dezube BJ, Crumpacker CS, Pardee AB. Three inhibitors of type 1 immunodeficiency virus long terminal repeat-directed gene expression and virus replication. Proc Natl Acad Sci USA 1993; 90:1839–1842. 55. Mazumder A, Raghavan K, Weinstein J, Kohn KW, Pommier Y. Inhibition of human immunodeficiency virus type-1 integrase by curcumin. Biochem Pharmacol 1995; 49:1165–1170. 56. Mazumder A, Gupta M, Perrin DM, Sigman DS, Rabinovitz M, Pommier Y. Inhibition of human immunodeficiency virus type 1 integrase by a hydrophobic cation: The phenanthroline-cuprous complex. AIDS Res Human Retro 1995; 11:115–125. 57. Mazumder A, Cooney D, Agbaria R, Gupta M, Pommier Y. Inhibition of human immunodeficiency virus type 1 integrase by 3' -azido-3' -deoxythymidylate. Proc Natl Acad Sci USA 1994; 91:5771–5775. 58. Ojwang J, Elbaggari A, Marshall HB, Jayaraman K, McGrath MS, Rando RF. Inhibition of human immunodeficiency virus type 1 activity in vitro by oligonucleotides composed entirely of guanosine and thymidine. J Acqu Immune Defic Syn 1994; 7:560–570. 59. Ojwang JO, Buckheit RW, Pommier Y, Mazumder A, de Vreese K, Esté JA, Reymen D, Pallansch LA, Lackman-Smith C, Wallace TL, de Clercq E, McGrath MS, Rando RF. T30177, an oligonucleotide stabilized by an intramolecular guanosine octet, is a potent inhibitor of laboratory strains and clinical isolates of human immunodeficiency virus type 1. Antimicrob Agents Chemother 1995; 39:2426–2435. 60. Carteau S, Mouscadet JF, Goulaouic H, Subra F, Auclair C. Inhibition of the in vitro integration of Moloney murine leukemia virus DNA by the DNA minor groove binder netropsin. Biochem Pharmacol 1994; 47:1821–1826. 61. Navia MA, Fitzgerald PMD, McKeever BM, Leu C-T, Heimbach JC, Herber WK, Sigal IS, Darke PL, Springer JP. Three-dimensional structure of aspartyl protease from human immunodeficiency virus HIV-1. Nature 1989; 337:615–620. 62. Wlodawer A, Erickson JW. Structure-based inhibitors of HIV-1 protease. Annu Rev Biochem 1993; 62:543–585. 63. Rice WG, Supko JG, Malspeis L, Buckheit Jr RW, Clanton D, Bu M, Graham L, Schaeffer CA, Turpin JA, Domagala J, Gogliotti R, Bader JP, Halliday SM, Coren L, Sowder II RC, Arthur LO, Henderson LE. Inhibitors of HIV nucleocapsid protein zinc fingers as candidates for the treatment of AIDS. Science 1995; 270:1194–1197. 64. Kalpana GV, Marmon S, Wang W, Crabtree GR, Goff SP. Binding and stimulation of HIV-1 integrase by a human homolog of yeast transcription factor SNF5. Science 1994; 266:2002–2006. http://legacy.netlibrary.com/nlreader/nlReader.dll?bookid=12640&filename=Page_117.html (1 of 2) [4/5/2004 4:56:01 PM]
Document 65. Gallay P, Swingler S, Song J, Bushman F, Trono D. HIV nuclear import is governed by the phosphotyrosine-mediated binding of matrix to the core domain of integrase. Cell 1995; 83:569–576. 66. Coffin JM. HIV population dynamics in vivo: Implications for genetic variation, pathogenesis, and therapy. Science 1995; 267:483–489. 67. Williams KJ, Loeb LA. Retroviral reverse transcriptases: Error frequencies and mutagenesis. Curr Top Microbiol Immunol 1992; 176:165–180. http://legacy.netlibrary.com/nlreader/nlReader.dll?bookid=12640&filename=Page_117.html (2 of 2) [4/5/2004 4:56:01 PM]
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Structure-based Drug Design 14 Stru
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Document 2 Structural Studies of HI
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Document Analysis of various HIV-1
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Document Page 54 Table 2) [12,54].
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Document Table 3 HIV-1 RT Amino Aci
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Document Page 72 16. Goldman ME, Nu
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Document 30. Coffin JM. HIV populat
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Document 45. Majumadar C, Abbotts J
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Document reverse transcriptase inhi
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Page 103 and 104: Document dine) and didanosine (dide
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Page 107 and 108: Document 163. Lacey SF, Larder BA.
Page 109 and 110: Document Figure 1 Retroviral lifecy
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Page 113 and 114: Document Page 88 transfer (Figure 3
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Page 117 and 118: Document Page 92 The role of the N-
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Page 135 and 136: Document Page 108 mulate during tre
Page 137 and 138: Document when metals are bound. Fin
Page 139 and 140: Document cubation of phosphotyrosin
Page 141 and 142: Document 4. Vink C, Plasterk RHA. T
Page 143 and 144: Document Page 115 21. Kulkosky J, J
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Page 149 and 150: Document 4 Bradykinin Receptor Anta
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Page 171 and 172: Document Page 141 receptor with int
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Page 179 and 180: Document 16. Martorana PA, Kettenba
Page 181 and 182: Document 39. Mavunkel BJ, Lu Z, Kyl
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Page 187 and 188: Document We determined the structur
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Document IV. Drug Design Progressio
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Document Table 1 Inhibition Data fo
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Document Page 166 As predicated, th
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Document References 1. Parks RE Jr.
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Document 17. Ealick SE, Rule SA, Ca
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Document 6 Structural Implications
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Document Page 176 0.43 Å) as the c
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Document IX. S2' Interactions Page
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Document 7 Structure—Function Rel
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Document Important for the validity
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Document Figure 4 Amino acids impor
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Document III. Results and Discussio
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Document Page 202 269, and valine-2
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Document Figure 6 Structure of α h
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Document Page 205 enzyme and of phe
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Document Page 207 sure and the acti
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Document 29. Baker ME. Genealogy of
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Document 31. Kettner C, Shaw E. D-P
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Document 12 Polypeptide Modulators
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Document 17. Szelke M. Chemistry of
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Document 65. João HC, Williams RJP
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Document 16 Progress in the Design
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Document Page 398 with growth hormo
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Document All effects of the IL-1 fa
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Document Figure 11 Functional resid
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Document 5. Dinarello CA. On the Bi
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Document 21. Seckinger P, Lowenthal
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Document 39. Saurat JH, Schfferli J
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Document 74. Bender PE, Lee JC., ed
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Document 102. Machin PJ, Osbond JM,
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Document 17 Structure and Functiona
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Document Table 1 Approval Indicatio
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Document Page 438 proteins. One pot
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Document II. Type IFNs A great deal
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Document Page 441 sequence of the m
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Document Page 443 that allowed for
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Document Figure 4 Stereo view of IF
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Document Figure 5 Velcro-key model
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Document Figure 6 Proposed receptor
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Document Page 451 with the cytoplas
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Document for directed subcellular t
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Document 13. Stewart HJ, McCann SHE
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Document Page 462 strains of influe
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Document Page 464 could not again b
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Document Figure 3 (a) A MOLSCRIPT [
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Document B. Protein Structure Page
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Document Figure 5 (a) Stereo image
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Document Page 471 molecules in the
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Document hydroxy, and 6 Neu5Ac2en -
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Document Figure 8 Stereo image of t
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Document Page 476 nM, respectively.
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Document Page 478 lished—was asso
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Document VI. Conclusion Page 480 It
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Document 21. Both GW, Sleigh MJ, Co
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Document 40. Drzenick R, Frank H, R
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Document 45. Varghese JN, Laver WG,
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Document 64. Ward CW, Elleman TC, A
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Document 80. Suzuki Y, Sato K, Kiso
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Document Page 486 95. Ryan DM, Tice
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Document Page 488 against most of t
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Document A. The Canyon Page 491 The
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Document Subsequent studies have sh
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Document Page 495 of the RNA and pr
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Document Figure 4 A ribbon diagram
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Document Figure 5 Some compounds wh
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Document Figure 7 HRV14 VP1 hydroph
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Document Page 514 sis. Large number
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Document Page 545 protein binding s
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Document Page 555 N-acylpyrrolidine
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Document 10. Bobbyer DNA, Goodford
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Document 30. O'Shea EK, Rutkowski R
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Document Acknowledgments Page 620 I
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Document 18. Sawyer TK. In: Peptide
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Document 97; (e) Fujii I, Nakamura
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Document Med Biol 1991; 306:9-21; (
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Document Page 629 ML, Clare M, Decr
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Document Page 631 197. Musil D, Zuc
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Document son AH, Drummond AH, Huxle
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Document Cyclotheonamide A (CtA), 2
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Document D ddI, 152 tumour necrosis
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Document antistasin peptides, 281 c
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Document fragment-based programs, 5
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Document [Human immunodeficiency vi
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Document Kininogen, 119 high molecu
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Document RT inhibitor, 41, 56 Nonpe
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Document Phosphoglycerate kinase (P
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Document [Protease targets] serinyl
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